Antimicrobials V2 Flashcards
1
Q
Penicillin G is administed
A
IM or IV
2
Q
Penicillin V is administed
A
orally
3
Q
mechanism of penicillins
A
covalent binding to transpeptidases/PBPs, cross-linking, activation of autolysins
4
Q
penicillins are bacterio-
A
cidal
5
Q
block penicillin excretion with
A
probenecid
6
Q
most ICWS inhibitors exibit
A
time dependent cell killing
7
Q
clinical use: Pen G and Pen V
A
gram +
8
Q
clinical use: anti-staphylococcal penicillins
A
beta-lactamase resistant
HHEELPSS
H. flu, H. pylori, E. coli, Enterococci, Listeria, Proteus mirabilis, Salmonella, Shigella
9
Q
anti-staphylococcal penicillins
A
nafcillin, methicillin, isooxazolyl
10
Q
extended spectrum antibiotics
A
ampicillin, amoxacillin
11
Q
clinical use: extended spectrum penicillins
A
increased gram - activity
12
Q
anti-pseudomonal penicillins
A
ticarcillin, piperacillin, mezlocillin
13
Q
clinical use: anti-pseudomonal penicillins
A
effective against psuedomonas and some other gram -
14
Q
due to rapid emergence of resistance with pseudomonas, use anti-psuedomonal penicillins in combination with
A
aminoglycosides or fluoroquinolones
15
Q
adverse effects of penicillins
A
ampicillin rash
hypersensitivity: complete cross-linking
seizures w/ renal failure
16
Q
resistance to penicillins
A
inaccessible PBPs (MRSA or gram -)
B-lactamase production
17
Q
to reduced beta lactamase activity, administer penicillins with
A
b lactamase inhibitors
18
Q
b lactamase inhibitors
A
clavulanic acid (augmenin)
sulbactam
tazobactam
19
Q
clavulanic acid….
A
dramatically increases effects of pens
20
Q
mechanism of cephalosporins
A
b-lactams, similar to pens
21
Q
pen-sensitive patients may have cross reactivity with
A
cephalosporins
22
Q
cephalosporins are bacterio
A
cidal
23
Q
1st gen cephalosporins
A
cefazolin
cephalexin
24
Q
2nd gen cephalosporins
A
cefuroxime
cefotetan
cefactor
25
3rd gen cephalosporins
ceftriaxone
cefotaxime
ceftazidime
cefpdoxime
26
4th gen cephalosporins
cefepime
27
cefepime exhibits _______ resistance
cephalosporinase
28
clinical use: 1st gen cephalosporins
gram +
29
clinical use: 2nd gen cephalosporins
some gram -, less gram +
30
clinical use: 3rd gen cephalosporins
serious gram - resistant to other b-lactams
31
clinical use: 4th gen cephalosporins
pseudomonas and cephalosporinase resistance
32
adverse effects: cephalosporins
irritation from injection
renal toxicity- enhanced by aminoglycosides
hypersensitivity
vitamin K deficiency
33
what antibiotics gives the Disulfiram effect?
cefotetan, bleeding and platelet disorders
34
what antibiotics gives the Disulfiram effect?
cefotetan, bleeding and platelet disorders
35
mechanism: azteronam
b lactam
36
clinical use: aztreonam
psuedomonas B-lactamase resistant
37
can azteronam cross the blood brain barrier?
yes
38
do azteronam exibit cross reactivity in pen-sensitive patients?
no
39
mechanism: imipenem
b lactam
40
clinical use: imipenem
broad, gram + and -
41
can imipenem cross the blood brain barrier?
yes
42
administration: imipenem
IV only
43
what should you coadminister with Imipenem?
cilastatin
inactivated by renal peptidase
44
meropenem
dipeptidase resistant carbapenem
45
does imipenem exhibit cross reactivity with pen-sensitive patients?
yes but incidence is low
46
mechanism: vancomycin
inhibits transglycosylation
47
vancomycin is bacteri-
cidal for gram +
48
vancomycin works synergistically with
aminoglycosides
49
vancomycin is given IV for
systemic use
50
vancomycin is given orally for
C. diff
51
clinical use: vancomycin
MRSA
52
adverse effects: vancomycin
flushing syndrome
renal and oto toxicity esp w/ aminoglycosides
53
mechanism: fosfomycin
inhibits cytoplasmic step in cell wall precursor synthesis
inhibits MurA blocking PG synthesis
54
clinical use: fosfomycin
gram + and gram -
single dose therapy UTI
55
fosfomycin is synergistic with
b lactams
aminoglycosides
fluoroquinolones
56
adverse effect: bacitracin
nephrotoxic
57
administration: bacitracin
topical only
58
pharmacokinetics: fosfomycin
G6P transporter
59
mechanism: colistin
act as detergents
60
clinical use: colistin
gram -
61
administation: colistin
topical due to renal toxicity
62
colistin is used as salvage therapy for
acinetobacter, pseudomonas, enterobacterieae
63
mechanism: tetracycline
reversible binding to 30S subunit
64
tetracycline is bacterio-
static
65
what class chelate metal ions?
tetracycline
66
what class should not be administered with calcium products?
tetracycline
67
can tetracyclines cross the placenta?
yes
68
excretion of doxycline
fecal
69
excretion of most tetracycline
urine
70
clinical use: tetracycline
broad spectrum
mycoplasma, chlamydia, rickettsiae
lyme disease
71
adverse effects: tetracycline
GI irritation
superinfections
liver damage
photosensitization
calcium chelation
72
resistance to tetracyclines
mainly efflux pumps
altered ribosomal proteins
73
glycycycline
newest tetracycline
retain antibacterial spectrum but overcome resistance
74
tigecycline is
not effected by efflux pump
75
tigecycline comes with
FDA black box warning, very dangerous
76
macrolides
erythromycin, clarithromycin, azithromycin
77
do macrolides distribute to CNS?
no
78
can macrolides cross the placenta?
yes
79
excretion: macrolides
bile
80
administration: macrolides
oral and IV
81
clinical use: macrolides
gram +, some gram -
mycoplasma pneumoniae, legionnaire's, chlamydia
82
can macrolides be given to pen-sensitive patients?
yes
83
broad spectrum macrolides
azithromycin and clarithromycin
84
adverse effects: macrolides
GI distress
microsomal enzyme inhibition
hepatotoxicity
QT prolongation
85
resistance: macrolides
staph resistant
methylated rRNA
efflux pump
esterase
86
benefits of clarithromycin
less GI effects
longer half life
87
which macrolide has minimal P450 interactions?
azithromycin
88
clarithromycin and azithromycin have
better bioavailability
active against mycobacterium avium
89
mechanism: telithromycin
binds 50S subunit
90
pharmacokinetics: telithromycin
poor substrate for efflux
inhibits CYP3A4
91
excretion: telithromycin
bile and urine
92
clinical use: telithromycin
RTIs
93
adverse effects: telithromycin
PQ prolongation
94
mechanism: aminoglycosides
irreversible inactivation of 30S
95
administration: aminoglycosides
usually IV
96
where do aminoglycosides NOT distribute?
eye, CNS
97
aminoglycosides and fluoroquinolones exhibit
concentration dependent killing
98
clinical uses: aminoglycosides
gram -
99
aminoglycosides for psuedomonas
gentamycin --> tobramycin --> amikacin
**oldest to newest
100
older aminoglycosides
streptomycin, gentamycin
101
adverse effects: aminoglycosides
nephrotoxicity
ototoxicity
dose and time dependent
102
resistance: aminoglycosides
evolves rapidly if AG is used alone
increased bacterial metabolism
alteration in bacterial uptake
altered ribosomal target
103
mechanism: chloramphenicol
reversible inhibitor of protein synthesis
104
chloramphenicol is bacterio
static
105
does chloarmphenicol distribute to the CNS?
yes
106
excretion: chloramphenicol
urine
107
resistance: chloramphenicol
plasmid mediated
CAT
slow development
108
adverse effects: chloramphenicol
GI upset
anemia due to bone marrow depression
aplastic anemia (Irreversible and fatal)
Gray baby syndrome
inhibits CYP450
109
clindamycin is bacterio
static
110
mechanism: clindamycin
binds 50S subunit
111
does clindamycin distribute to the CNS?
no
112
clinical use: clindamycin
MRSA, endocarditis prophylaxis
113
adverse effects: clindamycin
GI upset, C. diff, superinfections, hepatotoxicity
114
streptogramins
quinupristin, dalfopristin
115
mechanism: streptogramins
peptide macrolactones- bind novel ribosomal subunits
116
administation: streptogramins
IV
117
excretion: streptogramins
mostly bile, some urine
118
streptogramins inhibit
CYP34A
119
clinical use: streptogramins
vancomycin and MDR MRSA
120
resistance: streptogramins
complete cross resistance between the two components
121
mechanism: linezolid
prevents formation of 70S ribosome
122
administration: linezolid
IV or oral
123
clinical use: linezolid
bactericidal against streptococci
bacteriostatic against staphylococci and enterococci
vancomycin resistant e. faecium
limited to MDR gram+
124
adverse effects: linezolid
bone marrow suppression, thrombocytopenia
125
mechanism: sulfonamides
inhibit folate synthesis, PABA analogs
126
sulfonamides are bacterio
static
127
administration: sulfonamides
oral
128
are sulfonamides distributed to the CNS?
yes
129
excretion: sulfonamides
urine
130
topical sulfonamide for burns
silver sulfadizine
131
sulfonamide for ulcerative colitis
sulfasalazine
132
sulfonamide for ulcerative colitis
sulfasalazine
133
combine sulfonamides with
trimethoprim
134
adverse effects: sulfonamides
allergic reactions
cross reaction with other sulfonamides
Stevens Johnson syndrome
hematuria
135
resistance: sulfonamides
too much PABA
loss of permeability
new form of dihydropteroate synthesis
136
mechanism: trimethoprim
block bacterial enzyme that converts dihydrofolate reductase to tetrahydrofolate
137
adverse effects: trimethoprim
megaloblastic anemia
leukopenia
granulocytopenia
138
co-trimoxazole
add typical sulfonamide effectds
139
AIDS patients treat for pneumocystits receiving co-trimoxazole have
higher incidence of adverse effects
140
mechanism: Fluoroquinolones
DNA gyrase inhibitors
topo II and topo IV
141
fluoroquinolones
ciprofloxacin, levofloxacin
142
fluoroquinolones excretion is blocked by
probenecid
143
clinical use: fluoroquinolones
gram -, esp GI and UTI
144
adverse effects: fluoroquinolones
GI upset
connective tissue disorder
headaches, dizziness, insomnia
abnormal LFTs
145
resistance: fluoroquinolones
mutated DNA gyrase
plasmid-mediated protection
decreased permeability
146
Nitrofurantoin
UTIs
no systemic effect, excreted in urine
147
adverse effects: nitrofurantoin
anorexia
GI upset
hemolytic anemia
148
resistance: nitrofurantoin
psuedomonas
149
isoniazid mechanism
blocks synthesis of mycolic acid cell wall
150
can isoniazid distribute to the CNS?
yes
151
isoniazid metabolism
slow acetylators
152
clinical use: isoniazid
prophylaxis: TB
combination therapy for TB with IPE
153
adverse effects: isoniazid
dose and duration dependent
hepatotoxicity
peripheral and central neuropathy (B6)
154
resistance: isoniazid
mutation of KatG gene
155
mechanism: rifampin
inhibits DNA dependent RNA polymerase
156
rifampin is bacterio
cidal
157
excretion: rifampin
bile
158
adverse effects: rifampin
induced of microsomal enzymes
hepatotoxic
flu-like syndrome
159
mechanism: ethambutol
inhibits synthesis of mycobacterial and cell wall glycan via blocking arabinosyltransferase
160
is ethambutol distributed to CNS?
yes
161
excretion: ethambutol
urine
162
adverse effects: ethambutol
dose dependent
optic neuritis, color blindess
163
resistance: ethambutol
rapid, use in combination
164
pyrazinamide is bacterio
static
165
mechanism: pyrazinamide
activated by mycobacterium, blocks membrane functions
166
resistance: pyrazinamide
rapid, use in combination
167
adverse effects: pyrazinamide
hyperuricemia-gout
hepatotoxicity
contraindicated in pregnancy
168
second line TB drugs
extreme cases
PAS, cycloserine, ethionamide
169
dapsone
leprosy, p. jirovecii
170
hepatotoxicity ICE T
Isoniazid
Clindamycin
Erythromycin
Tetracycline
171
Ototoxicity: VA
vancomycin
aminoglycosides
172
renal toxicity: CAVS
Cavities in Kidneys
cephalosporins
aminoglycosides
vancomycin
sulfonamides
173
DOC H. flu
3rd gen cephalosporin
174
DOC rickettsia/lyme disease
doxycycline
175
DOC legionella
erythromycin, macrolides
176
DOC m. tuberculosis
RIPE
177
DOC M. pneumoniae
macrolides
178
DOC C. diff
vancomycin
179
pneumonia outpatient therapy healthy adults without risk
doxycycline, amoxicillin
***macrolide monotherapy (z pack) no longer recommended for S. pneumoniae
180
pneumonia outpatient therapy adults with risk factors
amoxicillin/clavulanate OR
cephalosporin AND macrolide or doxycycline OR
fluoroquinolone alone
181
pneumonia inpatient therapy no risk factors
ampicillin sulbactam OR
cephalosporin and macrolide OR
fluroquinolone alone
182
pneumonia inpatient therapy, no risk factor BUT contraindication to macrolides and fluoroquinolones
beta lactam OR cephalosporin
AND doxycycline
183
pneumonia inpatient therapy, risk for MRSA
vancomycin, linezolid
184
pneumonia inpatient therapy, risk for Psuedomonas
piperacillin tazobactam
cefepime or carbapenems
